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Tumour interposition suppository norcantharidin-alginic acid/poly-acid anhydride control-release microsphere

A technology of demethylcantharidin and alginic acid, applied in medical science, surgery, etc., can solve the problems of large blood vessel irritation, toxic and side effects, unstable drug release, etc., and achieve stable drug release, simple preparation process, and ball formation good sex effect

Inactive Publication Date: 2008-01-23
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used embolic agents in clinical interventional therapy are lipiodol and gelatin sponge, but medical practice shows that they have the following defects: lipiodol has poor compatibility with chemotherapy drugs, and drug release is unstable; gelatin sponge can only embolize to the hepatic artery 2-3 After embolization, collateral circulation is easy to establish, resulting in incomplete necrosis of cancer tissue and toxic side effects of chemotherapy drugs, resulting in significant short-term curative effect of interventional therapy for liver cancer, but unsatisfactory long-term curative effect, and the 5-year survival rate is only 6%. %about
However, norcantharidin is slightly soluble in water, and has great vascular irritation, so it is difficult to administer intravenously, and its oral bioavailability is low; some studies have used it for local injection treatment of liver cancer, but when the dose increases, the toxicity is still obvious , thus limiting its application in the clinical treatment of liver cancer

Method used

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  • Tumour interposition suppository norcantharidin-alginic acid/poly-acid anhydride control-release microsphere
  • Tumour interposition suppository norcantharidin-alginic acid/poly-acid anhydride control-release microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of norcantharidin-alginic acid / polyanhydride microspheres

[0026] PLGA and norcantharidin were simultaneously dissolved in ethyl acetate, and then emulsified with sodium alginate solution to form colostrum. The colostrum is emulsified with n-octane at a high speed, adding an emulsifier to adjust the HLB value to form double emulsion, then adding 15% calcium chloride solution and stirring for 10 minutes to fully cross-link calcium ions and alginic acid, and solidify to form calcium alginate. Filter under reduced pressure, rinse with distilled water several times, and dry in a 37°C oven overnight under reduced pressure. Sieve and pack according to particle size, 60 Co irradiation sterilization, obtains the drug microsphere of the present invention.

[0027] The test results of the physical and chemical properties of the microspheres show that the microspheres are uniform in size and round in shape, and the 95% confidence limit of the particle diameter of th...

Embodiment 2

[0028] Embodiment 2 Preparation process optimization of norcantharidin-alginic acid / polyanhydride microspheres

[0029] The preparation method is the same as in Example 1. According to the preliminary test results affecting particle size and material recovery rate, select the concentration of PLGA, oil phase volume, double emulsification stirring speed and four factors of stirring time, each factor selects 3 levels, and press Orthogonal Design Table L 9 (3 4 ) to conduct experiments under the set conditions to optimize the process parameters.

[0030] Table 1 is the orthogonal experiment factor and level table A2B1C3D1.

[0031] Table 2. Orthogonal Design Table L 9 (3 4 ) Experiment arrangement. .

[0032] Table 1.

[0033]

[0034] Table 2.

[0035] Test number

[0036] For the optimization method of microsphere preparation, encapsulation efficiency, particle size, in vitro drug release (including burst release effect) and material recovery were us...

Embodiment 3

[0043] Example 3 Effect of Alginic Acid and Polyanhydride Ratio on the Properties of Microspheres

[0044] Microspheres were prepared according to the ratio of alginic acid and polyanhydride in Table 5, and the method was the same as in Example 1.

[0045] Table 5. The ratio of alginic acid and polyanhydride to norcantharidin microspheres

[0046]

[0047] The results showed that; with the increase of alginic acid dosage, both drug and particle size increased. The reason for the analysis is that the increase in the amount of alginic acid increases the viscosity of the colostrum, making it difficult to form smaller complex emulsion droplets in the next step of emulsification. However, the viscosity of alginic acid increases, which obviously affects its yield.

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Abstract

The invention belongs to the pharmaceutical preparation filed and relates to a tumor interventional embolization agent, which takes norcantharidin as the active ingredient and biodegreadable material aliginate and polyanhydride as the accessories to establish emulsion-chemical crossline preparation method and prepare norcantharidin-alginic acid / poly acid anhydride micro-spheres. The norcantharidin micro spheres are applied for tumor interventional treatment through the hepatic artery. It can keep embolizing the tumor as long as one month and cause the tumor necrosis. At the same time, the microspheres can targetingly disperse in the tumor tissues to release the medicine slowly, prolong the active time of the medicine to the tumor tissues, increase partial medicine density and decrease the tumor toxicity. The invention has the advantages of targeting dispersed microspheres in the tumor tissues, long time for embolization, slow drug release, high anti-cancer effect and security.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a tumor intervention embolization agent, in particular to a tumor intervention embolization agent norcantharidin-alginic acid / polyanhydride controlled-release microspheres. Background technique [0002] Clinically, interventional therapy is the first choice for unresectable liver cancer. In 1950, klop pioneered hepatic arterial infusion chemotherapy, creating a precedent for interventional therapy for liver cancer. On this basis, Kato further developed transarterial chemoembolization (TACE), which pushed the curative effect of liver cancer to a new level. In China, interventional therapy has been widely used clinically since Lin Gui first carried out hepatic arterial embolization chemotherapy in 1984. Commonly used embolic agents in clinical interventional therapy are lipiodol and gelatin sponge, but medical practice shows that they have the following defects: lipiodol h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L31/16A61L31/04
Inventor 李琦范忠泽刘晓华孙珏李先茜殷佩浩王炎高虹
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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